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WO2005079784A1 - Nouvelles utilisations d'inhibiteurs de la cholinesterase - Google Patents

Nouvelles utilisations d'inhibiteurs de la cholinesterase Download PDF

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Publication number
WO2005079784A1
WO2005079784A1 PCT/EP2005/001715 EP2005001715W WO2005079784A1 WO 2005079784 A1 WO2005079784 A1 WO 2005079784A1 EP 2005001715 W EP2005001715 W EP 2005001715W WO 2005079784 A1 WO2005079784 A1 WO 2005079784A1
Authority
WO
WIPO (PCT)
Prior art keywords
composition according
treatment
vascular depression
administering
subject
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/EP2005/001715
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English (en)
Inventor
Roger Michael Lane
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Novartis Pharma GmbH Austria
Novartis AG
Original Assignee
Novartis Pharma GmbH Austria
Novartis AG
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34886209&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=WO2005079784(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority to CA002555386A priority Critical patent/CA2555386A1/fr
Priority to BRPI0507859-8A priority patent/BRPI0507859A/pt
Priority to AU2005215134A priority patent/AU2005215134B2/en
Priority to JP2006553554A priority patent/JP2007523121A/ja
Priority to US10/597,946 priority patent/US20070166363A1/en
Application filed by Novartis Pharma GmbH Austria, Novartis AG filed Critical Novartis Pharma GmbH Austria
Priority to EP05728652A priority patent/EP1718291A1/fr
Publication of WO2005079784A1 publication Critical patent/WO2005079784A1/fr
Anticipated expiration legal-status Critical
Priority to US12/707,691 priority patent/US20100184743A1/en
Priority to US12/868,595 priority patent/US20110021502A1/en
Ceased legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/70Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7023Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/27Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, meprobamate, carbachol, neostigmine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4453Non condensed piperidines, e.g. piperocaine only substituted in position 1, e.g. propipocaine, diperodon
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Definitions

  • the invention relates to the use of cholinesterase inhibitors in treating vascular depression.
  • the invention relates to the area of neurodegenerative diseases and, more particularly, to the treatment of vascular depression.
  • Vascular depression may be diagnosed from a combination of depressive ideation, greater psychomotor disturbance, apathy, executive dysfunction on neuropsychological testing, neuroimaging abnormalities in the basal ganglia and white matter on MRI. Damage to end-arteries supplying subcortical-striato-palido-thalamo-cortical pathways may disrupt neurotransmitter circuitry involved in mood regulation, thus causing or inducing depression. Potentially, this may occur either via strategically placed infarcts, particularly affecting thalamocortical projections, or is the result of an overall threshold effect.
  • vascular depression and subcortical vascular dementia may mean that the response of depressive symptoms to rivastigmine in patients with subcortical vascular dementia [see Moretti et al. (2002), supra] suggests that rivastigmine, and possibly other cholinesterase inhibitors, may be useful as monotherapy or augmentation agents in vascular depression with evidence of subcortical vascular pathology.
  • Cholinesterase inhibitors including the aforementioned rivastigmine, are useful in treating a number of physiological disorders responsive to the activation of acetyl choline receptors, e.g., senile dementia, Alzheimer's Disease, Huntingdon's chorea, tardive . ⁇ dyskinesias, hyperkinesias, mania, acute confusion disorder, Down's syndrome, Friedrich's ataxia, multiple sclerosis and vascular dementia.
  • senile dementia e.g., Alzheimer's Disease, Huntingdon's chorea, tardive . ⁇ dyskinesias, hyperkinesias, mania, acute confusion disorder, Down's syndrome, Friedrich's ataxia, multiple sclerosis and vascular dementia.
  • senile dementia e.g., Alzheimer's Disease, Huntingdon's chorea
  • tardive . ⁇ dyskinesias e.g., hyperkinesias
  • mania e.g., acute confusion disorder,
  • the present invention relates to the use of cholinesterase inhibitors for treating vascular depression.
  • the invention relates to the use of a cholinesterase inhibitor in the monotherapy treatment of vascular depression, preferably in the monotherapy treatment of late-onset vascular depression.
  • the invention relates to the use of a cholinesterase inhibitor in augmenting the anti-depressant therapy of vascular depression, preferably to augment the anti-depressant therapy of late-onset vascular depression.
  • the present invention is directed to a method of treating vascular depression utilizing a cholinesterase inhibitor.
  • the invention is directed to a method of treating vascular depression comprising administering to a subject in need of such treatment a therapeutically effective amount of a cholinesterase inhibitor.
  • the invention is directed to a method of treating late-onset vascular depression.
  • the invention relates to the use of cholinesterase inhibitors for the manufacture of medicaments for the treatment of vascular depression, preferably late-onset vascular depression.
  • the invention relates to pharmaceutical compositions comprising, in combination, a cholinesterase inhibitor and an anti-depressant. More particularly, said embodiment relates to a pharmaceutical composition comprising a pharmaceutically acceptable carrier or diluent and a therapeutically effective amount of: 1 ) a cholinesterase inhibitor; and 2) an anti-depressant.
  • the invention is directed to a method of treating vascular depression comprising administering to a subject in need of such treatment a therapeutically effective amount of a composition comprising, in combination, a cholinesterase inhibitor and at least one anti-depressant.
  • a composition comprising, in combination, a cholinesterase inhibitor and at least one anti-depressant.
  • the invention is directed to the use of said combination in treating late-onset vascular depression.
  • cholinesterase inhibitors are those set forth in USP 4,948,807, more preferably rivastigmine tartrate; USP 4,895,841, more preferably donepezil hydrochloride; and USP 4,663,318, more preferably galanthamine hydrobromide.
  • rivastigmine tartrate can be administered in tablet or capsule form or as a liquid oral concentrate under the tradename Exelon ® in a total daily dosage of between 3 mg and 12 mg.
  • rivastigmine can be administered transdermally in free base form, preferably via a transdermal patch of between 2 and 20 square centimeters (cm 2 ).
  • rivastigmine can be administered at a dose of 9 mg in a patch of ⁇ 5 cm 2 or at a dose of 18 mg in a patch of ⁇ 10 cm 2 , once every day.
  • donepezil hydrochloride can be administered in tablet form under the tradename Aricept ® in a total daily dosage of between 5 mg and 10 mg; and galanthamine bromide can be administered in tablet form under the tradename Reminyl ® in a total daily dosage of between 12 mg and 24 mg, e.g., 12 mg twice a day.
  • the above-mentioned cholinesterase inhibitors can be utilized to augment the anti-depressant therapy in treating vascular depression.
  • they can be utilized to augment: 1) the SSRI anti-depressants, viz., Paxil ® , Prozac ® , Zoloft ® , Celexa ® , Lexapro ® , etc.; 2) the SNRI anti-depressants, viz., Effexor ® , etc.; 3) the MAO inhibitor anti- depressants, viz., Nardil ® , Parnate ® , etc.; 4) the tricyclic anti-depressants, viz., Elavil ® , Norpramin ® , etc.; and 5) other anti-depressants which work somewhat differently, viz., Wellbutrin ® and Remeron ® .
  • the appropriate dosage of anti-depressants will, of course, vary depending upon, e.g., the compound employed, the host, the mode of administration and the nature and severity of the condition being treated. However, in general, satisfactory results are obtained when the anti-depressant is administered in the form that is marketed.
  • Paxil ® can be administered in tablet form in a total daily dosage of between 10 mg and 50 mg;
  • Prozac ® can be administered in tablet form in a total daily dosage of 20 mg;
  • Zoloft ® can be administered in tablet form in a total daily dosage of between 25 mg and 200 mg;
  • Celexa ® can be administered in tablet form in a total daily dosage of between 10 mg and 40 mg;
  • Lexapro ® can be administered in tablet form at a total daily dosage of between 10 mg and 20 mg;
  • Effexor ® can be administered in tablet form at a daily dosage of between 25 mg and 100 mg;
  • Nardil ® can be administered in tablet form at a total daily dosage of 15 mg;
  • Parnate ® can be administered in tablet form at a total daily dosage of 10 mg;
  • Elavil ® which is now marketed as amitriptyline, can be administered in tablet form at a total daily dosage of between 10 mg and 150 mg;
  • Norpramin ® can be administered in
  • the present invention also pertains to a pharmaceutical composition
  • a pharmaceutical composition comprising, in combination, a cholinesterase inhibitor and an anti-depressant
  • a pharmaceutical composition comprising, in combination, a cholinesterase inhibitor selected from Exelon ® , Aricept ® and Reminyl ® and an anti-depressant selected from SSRI anti- depressants, SNRI anti-depressants, MAO inhibitor anti-depressants, tricyclic anti- depressants, Wellbutrin ® and Remeron ®
  • a pharmaceutical composition comprising, in combination, a cholinesterase inhibitor selected from Exelon ® , Aricept ® and Reminyl ® and an anti-depressant selected from Paxil ® , Prozac ® , Zoloft ® , Celexa ® , Lexapro ® , Effexor ® , Nardil ® , Parnate ® , amitriptyline, Norpramin
  • the cholinesterase inhibitor and the anti-depressant may be present in free form or in the form of a pharmaceutically acceptable salt together with a pharmaceutically acceptable carrier or diluent for simultaneous, separate or sequential use in treating vascular depression.
  • the active ingredients of the above compositions may also be part of a "kit" in the sense that the active ingredients can be dosed independently or by use of different fixed combinations with distinct amounts of the active ingredients, i.e., simultaneously or at different times.
  • the parts of the kit can then, e.g., be administered simultaneously or chronologically staggered, that is at different time points and with equal or different time intervals for each component of the kit.
  • the time intervals are chosen such that the effect on the treated disease in the combined use of the parts is larger than the effect which would be obtained by use of only any one of the active ingredients.
  • the present invention also provides a commercial package comprising a combination as disclosed herein together with instructions for simultaneous or sequential use thereof in the treatment of vascular depression, preferably late-onset vascular depression.
  • a preferred commercial package is one wherein one of the active ingredients is Exelon ® .

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  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Emergency Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Medicinal Preparation (AREA)

Abstract

L'invention porte sur l'utilisation d'inhibiteurs de la cholinestérase pour traitement la dépression vasculaire.
PCT/EP2005/001715 2004-02-19 2005-02-18 Nouvelles utilisations d'inhibiteurs de la cholinesterase Ceased WO2005079784A1 (fr)

Priority Applications (8)

Application Number Priority Date Filing Date Title
EP05728652A EP1718291A1 (fr) 2004-02-19 2005-02-18 Nouvelles utilisations d'inhibiteurs de la cholinesterase
BRPI0507859-8A BRPI0507859A (pt) 2004-02-19 2005-02-18 uso dos inibidores da colinesterase
AU2005215134A AU2005215134B2 (en) 2004-02-19 2005-02-18 Use of cholinesterase inhibitors for treating vascular depression
JP2006553554A JP2007523121A (ja) 2004-02-19 2005-02-18 血管性鬱病の処置のためのコリンエステラーゼ阻害剤の使用
US10/597,946 US20070166363A1 (en) 2004-02-19 2005-02-18 Use of cholinesterase inhibitors for treating vascular depression
CA002555386A CA2555386A1 (fr) 2004-02-19 2005-02-18 Nouvelles utilisations d'inhibiteurs de la cholinesterase
US12/707,691 US20100184743A1 (en) 2004-02-19 2010-02-18 Use of cholinesterase inhibitors for treating vascular depression
US12/868,595 US20110021502A1 (en) 2004-02-19 2010-08-25 Use of cholinesterase inhibitors for treating vascular depression

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US54587104P 2004-02-19 2004-02-19
US60/545,871 2004-02-19

Related Child Applications (1)

Application Number Title Priority Date Filing Date
US12/707,691 Continuation US20100184743A1 (en) 2004-02-19 2010-02-18 Use of cholinesterase inhibitors for treating vascular depression

Publications (1)

Publication Number Publication Date
WO2005079784A1 true WO2005079784A1 (fr) 2005-09-01

Family

ID=34886209

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2005/001715 Ceased WO2005079784A1 (fr) 2004-02-19 2005-02-18 Nouvelles utilisations d'inhibiteurs de la cholinesterase

Country Status (10)

Country Link
US (3) US20070166363A1 (fr)
EP (1) EP1718291A1 (fr)
JP (1) JP2007523121A (fr)
KR (1) KR20060127136A (fr)
CN (1) CN1921844A (fr)
AU (1) AU2005215134B2 (fr)
BR (1) BRPI0507859A (fr)
CA (1) CA2555386A1 (fr)
RU (1) RU2397762C2 (fr)
WO (1) WO2005079784A1 (fr)

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007034990A1 (fr) * 2005-09-22 2007-03-29 Eisai R & D Management Co., Ltd. Nouvelle combinaison de medicaments utilises comme antidepresseur
WO2008019431A1 (fr) * 2006-08-14 2008-02-21 Brc Operations Pty Limited Procédé et compositions pour réguler simultanément la mémoire et l'humeur
WO2008033754A3 (fr) * 2006-09-11 2009-02-19 Univ Duke Méthodes et compositions de traitement de la dépression vasculaire.
EP2292219B1 (fr) 2005-12-01 2013-06-12 Novartis AG Système thérapeutique transdermal pour l'administration de rivastigmine
US20130289019A1 (en) * 2012-04-26 2013-10-31 Amazing Grace, Inc. Methods of treating behaviorial and/or mental disorders

Families Citing this family (3)

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Publication number Priority date Publication date Assignee Title
AR076590A1 (es) * 2009-05-19 2011-06-22 Vivia Biotech Sl Metodos para proveer pruebas medicinales personalizada ex vivo para neoplasmas hematologicos
US20100178307A1 (en) * 2010-01-13 2010-07-15 Jianye Wen Transdermal anti-dementia active agent formulations and methods for using the same
CN110354167A (zh) * 2019-09-02 2019-10-22 江西省科学院生物资源研究所 樟树提取物在抑制胆碱酯酶活性中的应用

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Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007034990A1 (fr) * 2005-09-22 2007-03-29 Eisai R & D Management Co., Ltd. Nouvelle combinaison de medicaments utilises comme antidepresseur
EP2292219B1 (fr) 2005-12-01 2013-06-12 Novartis AG Système thérapeutique transdermal pour l'administration de rivastigmine
DK201300015Y4 (da) * 2005-12-01 2016-02-12 Novartis Ag Transdermalt terapeutisk system
DK201600113Y4 (da) * 2005-12-01 2017-06-09 Novartis Ag Transdermalt, terapeutisk system til administration af rivastigmin
WO2008019431A1 (fr) * 2006-08-14 2008-02-21 Brc Operations Pty Limited Procédé et compositions pour réguler simultanément la mémoire et l'humeur
WO2008033754A3 (fr) * 2006-09-11 2009-02-19 Univ Duke Méthodes et compositions de traitement de la dépression vasculaire.
US20130289019A1 (en) * 2012-04-26 2013-10-31 Amazing Grace, Inc. Methods of treating behaviorial and/or mental disorders

Also Published As

Publication number Publication date
RU2006133263A (ru) 2008-03-27
AU2005215134A1 (en) 2005-09-01
US20110021502A1 (en) 2011-01-27
BRPI0507859A (pt) 2007-07-17
RU2397762C2 (ru) 2010-08-27
US20100184743A1 (en) 2010-07-22
KR20060127136A (ko) 2006-12-11
EP1718291A1 (fr) 2006-11-08
CA2555386A1 (fr) 2005-09-01
JP2007523121A (ja) 2007-08-16
AU2005215134B2 (en) 2009-01-29
US20070166363A1 (en) 2007-07-19
CN1921844A (zh) 2007-02-28

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